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Sotuletinib hydrochloride {[allProObj[0].p_purity_real_show]}

货号:A1977887 同义名: BLZ945 hydrochloride Ambeed 开学季,买赠积分,赢豪礼

Sotuletinib hydrochloride是一种高效、选择性且具有脑渗透性的 CSF-1R (c-Fms) 抑制剂,IC50 为 1 nM。其对其他受体酪氨酸激酶同系物的选择性高出 1000 倍,适用于神经退行性疾病和肿瘤微环境的研究。

Sotuletinib hydrochloride 化学结构 CAS号:2222138-31-8
Sotuletinib hydrochloride 化学结构
CAS号:2222138-31-8
Sotuletinib hydrochloride 3D分子结构
CAS号:2222138-31-8
Sotuletinib hydrochloride 化学结构 CAS号:2222138-31-8
Sotuletinib hydrochloride 3D分子结构 CAS号:2222138-31-8
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Sotuletinib hydrochloride 纯度/质量文件 产品仅供科研

货号:A1977887 标准纯度: {[allProObj[0].p_purity_real_show]}
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Sotuletinib hydrochloride 生物活性

描述 Sotuletinib (BLZ945) hydrochloride acts as a potent, selective, and brain-penetrating inhibitor of CSF-1R (c-Fms), demonstrating an IC50 of 1 nM. It exhibits over 1,000-fold selectivity compared to its nearest receptor tyrosine kinase relatives[1].
体内研究

Mice receiving Sotuletinib hydrochloride or a vehicle are monitored for symptom-free survival, with the vehicle group showing a median survival of 5-7 weeks. Remarkably, Sotuletinib hydrochloride markedly extends long-term survival, with 64.3% of subjects alive at the 26-week trial conclusion, a duration chosen due to spontaneous tumor development in Ink4a/Arf / mice around ~30 weeks. Sotuletinib hydrochloride demonstrates a high tolerance in prolonged treatment without noticeable side effects, aligning with histopathological findings. Histological analysis shows all vehicle-treated mice developed high-grade, invasive gliomas, whereas Sotuletinib hydrochloride treatment results in significantly less malignant tumors, with 55.6% of asymptomatic mice showing no detectable lesions at the trial's end[1].

Mice treated with Sotuletinib hydrochloride exhibit decreased CSF1R staining in cervical tumors and their surrounding stroma, demonstrating a notable reduction in CSF1R+ stromal macrophages compared to those treated with the vehicle (P<0.05)[2].

体外研究

Sotuletinib hydrochloride suppresses CSF-1-induced proliferation (EC50=67 nM) in bone marrow-derived macrophages (BMDMs) and reduces CSF-1R phosphorylation, akin to CSF-1R antibody inhibition. It also lowers the viability of CRL-2467 microglia, Ink4a/Arf / BMDMs (PDG genetic background), and NOD/SCID BMDMs. Notably, in vitro treatment with Sotuletinib hydrochloride does not influence the proliferation of PDG-derived tumor cell lines (all Csf-1r-negative), U-87 MG human glioma cells, or affect PDG cell tumor sphere formation. Therefore, Sotuletinib hydrochloride directly targets macrophage survival via CSF-1R blockade without impacting glioma cells[1].

Sotuletinib hydrochloride 参考文献

[1]Pyonteck SM, et al. CSF-1R inhibition alters macrophage polarization and blocks glioma progression. Nat Med. 2013 Oct;19(10):1264-72.

[2]Strachan DC, et al. CSF1R inhibition delays cervical and mammary tumor growth in murine models by attenuating the turnover of tumor-associated macrophages and enhancing infiltration by CD8+ T cells. Oncoimmunology. 2013 Dec 1;2(12):e26968.

Sotuletinib hydrochloride 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.30mL

0.46mL

0.23mL

11.50mL

2.30mL

1.15mL

22.99mL

4.60mL

2.30mL

Sotuletinib hydrochloride 技术信息

CAS号2222138-31-8
分子式C20H23ClN4O3S
分子量 434.94
别名 BLZ945 hydrochloride
运输蓝冰
存储条件

粉末 Inert atmosphere,Room Temperature

液体 -20°C:3-6个月-80°C:12个月

溶解度

DMSO: 105 mg/mL(241.41 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

H2O: 100 mg/mL(229.92 mM),配合低频超声助溶

动物实验配方
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